Home Autophagy LRRK2 inhibitor PF-06447475 For research use only.

PF-06447475

PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM.

PF-06447475 Chemical Structure

PF-06447475 Chemical Structure

CAS: 1527473-33-1

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Choose Selective LRRK2 Inhibitors

Biological Activity

Description PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM.
Targets
LRRK2 [1]
(Cell-free assay)		 G2019S LRRK2 [1]
(Cell-free assay)
3nM 11nM
In vitro
In vitro In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. [2] In astrocytes, PF-06447475 rescues LRRK2 mutation-induced defects in lysosomal morphology and function. [3]
In Vivo
In vivo In G2019S BAC-transgenic mice, PF-06447475 (100 mg/kg, p.o.) inhibits pS935 and pS1292 phosphorylation of LRRK2 with IC50 of 103 nM and 21 nM, respectively. [1] In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) blocks α-synuclein-induced dopaminergic neurodegeneration and attenuates neuroinflammation associated with G2019S-LRRK2 expression. [2]
Animal Research Animal Models G2019S BAC-transgenic mice
Dosages 100 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 305.33 Formula

C17H15N5O
CAS No. 1527473-33-1 SDF Download PF-06447475 SDF
Smiles C1COCCN1C2=NC=NC3=C2C(=CN3)C4=CC=CC(=C4)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 61 mg/mL ( (199.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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